HRP20201147T1 - (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors - Google Patents

(2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors Download PDF

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Publication number
HRP20201147T1
HRP20201147T1 HRP20201147TT HRP20201147T HRP20201147T1 HR P20201147 T1 HRP20201147 T1 HR P20201147T1 HR P20201147T T HRP20201147T T HR P20201147TT HR P20201147 T HRP20201147 T HR P20201147T HR P20201147 T1 HRP20201147 T1 HR P20201147T1
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Croatia
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compound
formula
rhinitis
asthma
induced
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HRP20201147TT
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Croatian (hr)
Inventor
Hans Roland Lönn
Stephen Connolly
Steven Swallow
Staffan PO KARLSSON
Carl-Johan Aurell
John Fritiof PONTÉN
Kevin James Doyle
Amanda Jane Van De Poël
Graham Peter Jones
David Wyn Watson
Jacqueline Anne Macritchie
Nicholas John Palmer
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Astrazeneca Ab
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Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of HRP20201147T1 publication Critical patent/HRP20201147T1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Claims (7)

1. Spoj formule (I) [image] gdje R1 je [image] X je izabran od O, S ili CF2; R6 je izabran od C1-3alkila, pri čemu je navedeni C1-3alkil izborno supstituiran sa 1, 2 ili 3 F; R7 je izabran od vodika, F, Cl ili CH3; ili njegova farmaceutski prihvatljiva sol.1. Compound of formula (I) [image] where R1 is [image] X is selected from O, S or CF2; R 6 is selected from C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted with 1, 2 or 3 F; R 7 is selected from hydrogen, F, Cl or CH 3 ; or a pharmaceutically acceptable salt thereof. 2. Farmaceutska kompozicija koja sadrži spoj formule (I) prema patentnom zahtjevu 1 i farmaceutski prihvatljiv adjuvans, razblaživač ili nosač.2. A pharmaceutical composition containing a compound of formula (I) according to patent claim 1 and a pharmaceutically acceptable adjuvant, diluent or carrier. 3. Spoj formule (I) prema patentnom zahtjevu 1 za upotrebu u terapiji.3. Compound of formula (I) according to patent claim 1 for use in therapy. 4. Spoj formule (I) prema patentnom zahtjevu 1, za upotrebu u liječenju opstruktivnih bolesti dišnih puteva: uključujući bilo koju od astme, uključujući bronhijalnu, alergijsku, intrinzičnu, ekstrinzičnu, induciranu vježbanjem, induciranu lijekom (uključujući induciranu aspirinom i sa NSAID) i astmu induciranu prašinom, intermitetnu i perzistentnu i svih težina, i druge uzroke hiper-responsivnosti dišnih puteva; kroničnu opstruktivnu bolest pluća (COPD); bronhitis, uključujući infektivni i eozinofilni bronhitis; emfizem; bronhiektazu; cističnu fibrozu; sarkoidozu; deficijenciju alfa-1 antitripsina; pluća farmera i srodne bolesti; hipersenzitivni pneumonitis; fibrozu pluća, uključujući kriptogeni fibrozni alveolitis, idiopatske intersticijalne pneumonije, fibrozu koju komplicira anti-neoplastična terapija i kronična infekcija, uključujući tuberkulozu i aspergilozu i druge gljivične infekcije; komplikacije transplantacije pluća; vaskulitis i trombotičke poremećaje vaskulature pluća, i plućnu hipertenziju; antitusivnu aktivnost uključujući tretman kroničnog kašlja povezanog sa inflamatornim i sekretornim stanjima dišnih puteva, i jatrogeni kašalj; akutni i kronični rinitis uključujući rinitis medikamentozu, i vazomotorni rinitis; alergijski rinitis od višegodišnjih i sezonskih biljaka uključujući rinitis nervozu (peludnu groznicu); nazalnu polipozu; akutnu virusnu infekciju uključujući običnu prehladu, i infekciju kao posljedicu respiratornog sincicijalnog virusa, influencu, koronavirus (uključujući SARS) i adenovirus, akutnu ozljedu pluća, adultni respiratorni distres sindrom (ARDS), kao i pogoršanja svakog od gore navedenih stanja bolesti respiratornog trakta, naročito pogoršanja svih tipova astme ili COPD.4. A compound of formula (I) according to claim 1, for use in the treatment of obstructive airway diseases: including any of asthma, including bronchial, allergic, intrinsic, extrinsic, exercise-induced, drug-induced (including aspirin and NSAID-induced) and dust-induced asthma, intermittent and persistent and of all severity, and other causes of airway hyper-responsiveness; chronic obstructive pulmonary disease (COPD); bronchitis, including infectious and eosinophilic bronchitis; emphysema; bronchiectasis; cystic fibrosis; sarcoidosis; alpha-1 antitrypsin deficiency; farmer's lung and related diseases; hypersensitivity pneumonitis; pulmonary fibrosis, including cryptogenic fibrous alveolitis, idiopathic interstitial pneumonias, fibrosis complicated by anti-neoplastic therapy and chronic infection, including tuberculosis and aspergillosis and other fungal infections; complications of lung transplantation; vasculitis and thrombotic disorders of the lung vasculature, and pulmonary hypertension; antitussive activity including the treatment of chronic cough associated with inflammatory and secretory conditions of the airways, and iatrogenic cough; acute and chronic rhinitis, including rhinitis medicamentosa, and vasomotor rhinitis; allergic rhinitis from perennial and seasonal plants including rhinitis nervosa (hay fever); nasal polyposis; acute viral infection including the common cold, and infection as a result of respiratory syncytial virus, influenza, coronavirus (including SARS) and adenovirus, acute lung injury, adult respiratory distress syndrome (ARDS), as well as exacerbations of any of the above-mentioned respiratory tract disease conditions, especially exacerbations of all types of asthma or COPD. 5. Spoj formule (I) za upotrebu prema patentnom zahtjevu 4 za upotrebu u liječenju astme ili kronične opstruktivne bolesti pluća.5. A compound of formula (I) for use according to claim 4 for use in the treatment of asthma or chronic obstructive pulmonary disease. 6. Spoj formule (I) za upotrebu prema patentnom zahtjevu 4 za upotrebu u liječenju bronhiektaze.6. A compound of formula (I) for use according to claim 4 for use in the treatment of bronchiectasis. 7. Kombinacija spoja formule (I) prema patentnom zahtjevu 1 i jednog ili više sredstava nezavisno izabranih od: • nesteroidnog agonista receptora glukokoritokoida; • selektivnog agonista β2 adrenoceptora; • inhibitora fosfodiesteraze; • inhibitora proteaze; • glukokortikoida; • antiholinergičkog sredstva; • modulatora funkcije receptora za hemokin; i • inhibitora funkcije kinaze.7. Combination of the compound of formula (I) according to claim 1 and one or more agents independently selected from: • non-steroidal glucocorticoid receptor agonist; • selective β2 adrenoceptor agonist; • phosphodiesterase inhibitors; • protease inhibitors; • glucocorticoids; • anticholinergic agent; • modulator of chemokine receptor function; and • inhibitors of kinase function.
HRP20201147TT 2014-01-24 2020-07-23 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors HRP20201147T1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461931090P 2014-01-24 2014-01-24
EP17195612.1A EP3323814B1 (en) 2014-01-24 2015-01-23 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

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HRP20201147T1 true HRP20201147T1 (en) 2020-12-11

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HRP20180116TT HRP20180116T1 (en) 2014-01-24 2018-01-22 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors
HRP20201147TT HRP20201147T1 (en) 2014-01-24 2020-07-23 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

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US (16) US9522894B2 (en)
EP (3) EP3097086B1 (en)
JP (5) JP6469711B2 (en)
KR (1) KR102417684B1 (en)
CN (2) CN110483492B (en)
AP (1) AP2016009322A0 (en)
AR (1) AR099177A1 (en)
AU (4) AU2015208932C1 (en)
BR (1) BR112016016224B1 (en)
CA (1) CA2935625C (en)
CL (1) CL2016001889A1 (en)
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CY (2) CY1120049T1 (en)
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EA (1) EA032794B1 (en)
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HK (2) HK1225730B (en)
HR (2) HRP20180116T1 (en)
HU (2) HUE038274T2 (en)
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